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| | Suplatast tosilate Basic information |
| Product Name: | Suplatast tosilate | | Synonyms: | (2-(4-(3-ethoxy-2-hydroxypropoxy)phenylcarbamoyl)ethyl)dimethylsulfonium p-toluenesulfonate;2-[4-(2-Hydroxy-3-ethoxypropoxy)phenylcarbamoyl]ethyldimethylsulfonium·4-methylbenzenesulfonate;IPD-1151T;S,S-Dimethyl-3-oxo-3-[4-(2-hydroxy-3-ethoxypropoxy)anilino]propane-1-sulfonium·4-methylbenzenesulfonate;[2-[[[4-(2-Hydroxy-3-ethoxypropoxy)phenyl]amino]carbonyl]ethyl]dimethylsulfonium;[2-[4-(2-Hydroxy-3-ethoxypropoxy)phenylcarbamoyl]ethyl]dimethylsulfonium;[3-Oxo-3-[4-(2-hydroxy-3-ethoxypropoxy)phenylamino]propyl]dimethylsulfonium;2-[4-(2-Hydroxy-3-ethoxypropoxy)phenylcarbamoyl]ethyldimethylsulfonium | | CAS: | 94055-76-2 | | MF: | C23H33NO7S2 | | MW: | 499.64062 | | EINECS: | | | Product Categories: | API;Aromatics;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;IPD 1151T | | Mol File: | 94055-76-2.mol |  |
| | Suplatast tosilate Chemical Properties |
| Melting point | 84-87°C | | storage temp. | Inert atmosphere,Room Temperature | | solubility | DMSO: >20mg/mL | | form | powder | | color | white to off-white | | Merck | 14,9003 | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. | | CAS DataBase Reference | 94055-76-2(CAS DataBase Reference) |
| WGK Germany | 3 | | RTECS | WR7906000 | | HS Code | 2930.90.2900 | | Toxicity | LD50 in male, female mice, male, female rats (mg/kg): 81, 96, 96, 93 i.v.; in mice, rats (g/kg): >12.5, >10 orally (Yamashita) |
| | Suplatast tosilate Usage And Synthesis |
| Description | Suplatast tosylate is a unique dimethylsulfonium salt marketed in Japan
for the treatment of bronchial asthma, atopic dermatitis and allergic rhinitis. Suplatast
tosylate is a potent inhibitor of IgE synthesis without suppressing IgM and IgG. The
mechanism of action for suplatast tosylate is thought to be via the inhibition of
interleukin-4 and interleukin-6 production by T-cells at the gene level. In allergic
patients, suplatast tosylate markedly improved clinical symptoms which correlated with
a significant decrease in serum IgE antibody levels. | | Description | Suplatast is an antiallergic agent. It inhibits IL-4 and IL-5 production in conalbumin-stimulated D10.G4.1 murine T helper 2 (Th2) cells in a concentration-dependent manner. Suplatast (100 mg/kg) inhibits ovalbumin-induced increases in eosinophil and total cell numbers, as well as IL-4, IL-5, and IL-13, but not IFN-γ, levels in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of asthma. It also inhibits ovalbumin-induced increases in ovalbumin-specific IgE in serum and bronchial hyperresponsiveness to methacholine in the ovalbumin-sensitized mouse model of asthma. | | Originator | Taiho (Japan) | | Uses | Suplatast Tosylate is an antiallergic drug. Suplatast Tosylate inhibits antigen-induced histamine release from mast cells as well as IgE antibody formation. Suplatast Tosylate suppresses interleukin (IL)-4 release from T cells, however in human peripheral basophils, Suplatast Tosylate inhibited the antigen-induced release of IL-13 but not IL-4. | | Uses | Suplatast Tosilate is a novel capsular anti-asthmatic agent that suppresses both IgE production, IL-4 and IL-5 synthesis with IC50 above 100 μM. | | Brand name | IPD | | Biological Activity | Th2 cytokine inhibitor that attenuates IL-2, IL-5 and IL-13 production and has no effect on IFN- γ production. Acts as an immunoregulator that suppresses IgE production, eosinophil infiltration and histamine release. Exhibits antiasthmatic, anti-inflammatory and antifibrotic activity in vivo and is orally active. | | References | 1) Kurokawa?et al.?(2001),?Suppressive effects of anti-allergic agent suplatast tosilate (IPD-1151T) on the expression of co-stimulatory molecules on mouse splenocytes in vivo; Mediators Inflamm.,?10?333
2) Hsu?et al.?(2007),?The effects of suplatast tosilate (IPD-1151T) on innate immunity and antigen-presenting cells; Transpl. Immunol.,?18?108
3) Furonaka?et al.?(2009),?Suplatast tosilate prevents bleomycin-induced pulmonary fibrosis in mice; Curr. Opin. J. Pharmacol. Exp. Ther.,?328?55
4) Bhattachrya?et al.?(2014),?Simultaneous inhibition of T helper 2 and T regulatory cell differentiation by small molecules enhances Bacillus Calmette-Guerin vaccine efficacy against tuberculosis; J. Biol. Chem.,?289?33404
5) Wada?et al.?(2009),?Effect of suplatast tosilate on antileukotriene non-responders with mild-to-moderate persistent asthma; Allergol. Int.,?58?389 |
| | Suplatast tosilate Preparation Products And Raw materials |
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